Traditionally, in the dibenzocycloheptene series of compounds, those with a piperidinylidene group in the 5-position have been considered to be without notable antipsychotic action. Recently, however, 3-cyanocyproheptadine, and particularly the levorotatory enantiomer thereof was found to have antipsychotic activity.
Surprisingly, it has now been found that trifluoromethylthio and trifluoromethylsulfonyl derivatives of cyproheptadine carrying a hydroxyalkyl or cycloalkylalkyl group on the piperidine nitrogen are also potent antipsychotic agents, with a low propensity to induce extrapyramidal side effects.
The antipsychotic activity resides predominantly in the levorotatory enantiomers, whereas the dextrorotatory enantiomers, although lacking in antipsychotic activity, are anticholinergic agents. Each enantiomer is additionally useful as a source of the other by a process of racemization.
It is thus an object of the present invention to provide novel compounds which are potent antipsychotic agents with a very low propensity to induce the extrapyramidal side effects experienced with most major tranquilizers, and to provide novel compounds with anticholinergic activity.
It is a further object of this invention to provide novel processes for the preparation of the novel compounds.
Another object of the invention is to provide novel pharmaceutical compositions comprising the novel compounds as active ingredient.
Another object of the invention is to provide a novel method of treating psychoses by administration of the novel antipsychotic compounds or pharmaceutical compositions thereof to a patient.
Another object of this invention is to provide novel intermediates from which the pharmacologically active compounds are prepared